Page last updated: 2024-08-05 14:55:22

EC 3.1.1.8 (cholinesterase) inhibitor

An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of cholinesterase (EC 3.1.1.8).

ChEBI ID: 37733

Members (45)

MemberDefinitionClass
11-hydroxysugiolAn abietane diterpenoid that is sugiol in which the hydrogen ortho to the phenolic hydroxy group has been replaced by a hydroxy group.11-hydroxysugiol
alternariolA benzochromenone that is 6H-benzo[c]chromen-6-one which is substituted by a methyl group at position 1 and by hydroxy groups at positions 3, 7, and 9. It is the most important mycotoxin produced by the black mould Alternaria species, which are the most common mycoflora infecting small grain cereals worldwide.alternariol
ambenoniumA symmetrical oxalamide-based bis-quaternary ammonium ion having ethyl and 2-chlorobenzyl groups attached to the nitrogens.ambenonium
ambenonium chlorideA symmetrical oxalamide-based bis-quaternary ammonium salt having ethyl and 2-chlorobenzyl groups attached to the nitrogens.ambenonium chloride
azinphosmethylA member of the class of benzotriazines that is 1,2,3-benzotriazine substituted by an oxo group at position 4 and a [(dimethoxyphosphorothioyl)sulfanyl]methyl group at position 3.azinphos-methyl
berberineberberine
bupivacaine hydrochlorideA racemate composed of equimolar amounts of dextrobupivacaine hydrochloride and levobupivacaine hydrochloride. The monohydrate form is commonly used as a local anaesthetic.1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide hydrochloride; bupivacaine hydrochloride (anhydrous)
carbarylA carbamate ester obtained by the formal condensation of 1-naphthol with methylcarbamic acid.carbaryl
carbofurancarbofuran
chlorfenvinphoschlorfenvinfos
chlorpyrifosAn organic thiophosphate that is O,O-diethyl hydrogen phosphorothioate in which the hydrogen of the hydroxy group has been replaced by a 3,5,6-trichloropyridin-2-yl group.chlorpyrifos
coumaphoscoumaphos
diazinonA member of the class of pyrimidines that is pyrimidine carrying an isopropyl group at position 2, a methyl group at position 6 and a (diethoxyphosphorothioyl)oxy group at position 4.diazinon
dichlorvosAn alkenyl phosphate that is the 2,2-dichloroethenyl ester of dimethyl phosphate.dichlorvos
dimethoateA monocarboxylic acid amide that is N-methylacetamide in which one of the hydrogens of the methyl group attached to the carbonyl moiety is replaced by a (dimethoxyphosphorothioyl)sulfanediyl group.dimethoate
distigmineA carbamate ester resulting from the formal condensation of both carboxy groups of hexane-1,6-diylbis(methylcarbamic acid) with the hydroxy group of 3-hydroxy-1-methylpyridinium.distigmine
disulfiramAn organic disulfide that results from the formal oxidative dimerisation of N,N-diethyldithiocarbamic acid. A multi-enzyme inhibitor that is used in alcohol aversion therapy and also exhibits anticancer properties.disulfiram
donepezilA racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one; donepezil
echothiophate iodideThe iodide salt of ecothiopate. An irreversible acetylcholinesterase inhibitor, it is used an ocular antihypertensive in the treatment of open-angle glaucoma, particularly when other drugs have proved inadequate.ecothiopate iodide
edrophoniumA quaternary ammonium ion that is N-ethyl-N,N-dimethylanilinium in which one of the meta positions is substituted by a hydroxy group. It is a reversible inhibitor of cholinesterase, with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes). The chloride salt is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.edrophonium
edrophonium chlorideThe chloride salt of edrophonium. A reversible inhibitor of cholinesterase with a rapid onset (30-60 seconds after injection) but a short duration of action (5-15 minutes), it is used in myasthenia gravis both diagnostically and to distinguish between under- or over-treatment with other anticholinesterases. It has also been used for the reversal of neuromuscular blockade in anaesthesia, and for the management of poisoning due to tetrodotoxin, a neuromuscular blocking toxin found in puffer fish and other marine animals.edrophonium chloride
fenitrothionAn organic thiophosphate that is O,O-dimethyl O-phenyl phosphorothioate substituted by a methyl group at position 3 and a nitro group at position 4.fenitrothion
fenthionAn organic thiophosphate that is O,O-dimethyl hydrogen phosphorothioate in which the hydrogen atom of the hydroxy group is replaced by a 3-methyl-4-(methylsulfanyl)phenyl group. It exhibits acaricidal and insecticidal activities.fenthion
fonofosfonofos
galantamineA benzazepine alkaloid isolated from certain species of daffodils.galanthamine
levobupivacaineThe (S)-(-)-enantiomer of bupivacaine.levobupivacaine
levobupivacaine hydrochlorideThe monohydrochloride salt of levobupivacaine.levobupivacaine hydrochloride (anhydrous)
lucidenic acid nA tetracyclic triterpenoid that is 25,26,27-trinorlanost-8-en-24-oic acid substituted by hydroxy groups at positions 3 and 7 and oxo groups at positions 11 and 15 respectively (the 3beta,5alpha,7beta stereoisomer). Isolated from the fruiting bodies of Ganoderma lucidum, it exhibits cytotoxicity against tumour cells.lucidenic acid N
methomylA carbamate ester obtained by the formal condensation of methylcarbamic acid with the hydroxy group of 1-(methylsulfanyl)acetaldoxime.methomyl
methyl parathionA C-nitro compound that is 4-nitrophenol substituted by a (dimethoxyphosphorothioyl)oxy group at position 4.parathion-methyl
methylene blueAn organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.methylene blue
monocrotophosAn alkenyl phosphate that is the 4-(methylamino)-4-oxobut-2-en-2-yl ester of dimethyl phosphate.monocrotophos
naledAn dialkyl phosphate resulting from the formal condensation of the acidic hydroxy group of dimethyl hydrogen phosphate with the alcoholic hydroxy group of 1,2-dibromo-2,2-dichloroethanol. An organophosphate insecticide, it is no longer approved for use within the European Union.naled
neostigmine methylsulfateneostigmine methyl sulfate
nostocarbolineA member of the class of beta-carbolines that is 9H-beta-carbolin-2-ium substituted by a chloro group at position 6 and a methyl group at position 2. It is isolated from a fresh water cyanobacterium Nostoc 78-12A and acts as an inhibitor of butyrylcholinesterase.nostocarboline
parathionparathion
phoratephorate
phosaloneA member of the class of 1,3-benzoxazoles carrying a [(diethoxyphosphorothioyl)sulfanyl]methyl group at the nitrogen atom, an oxo group at position 2 and a chloro group at position 6. It is an organothiophosphate insecticide.phosalone
physostigminephysostigmine
prothiophosAn organic thiophosphate that is the 2,4-dichlorophenyl ester of O-ethyl S-propyl dithiophosphoric acid.prothiofos
rivastigmineA carbamate ester obtained by formal condensation of the carboxy group of ethyl(methyl)carbamic acid with the phenolic OH group of 3-[(1S)-1-(dimethylamino)ethyl]phenol. A reversible cholinesterase inhibitor.rivastigmine
sulfoteppsulfotep
tetrachlorvinphostetrachlorvinphos
trichlorfonA phosphonic ester that is dimethyl phosphonate in which the hydrogen atom attched to the phosphorous is substituted by a 2,2,2-trichloro-1-hydroxyethyl group.trichlorfon
tyramineA primary amino compound obtained by formal decarboxylation of the amino acid tyrosine.tyramine

Research

Studies (51,467)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199018,087 (35.14)18.7374
1990's5,803 (11.28)18.2507
2000's9,024 (17.53)29.6817
2010's12,772 (24.82)24.3611
2020's5,781 (11.23)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials2,920 (4.99%)5.53%
Reviews2,927 (5.00%)6.00%
Case Studies2,769 (4.73%)4.05%
Observational106 (0.18%)0.25%
Other49,832 (85.10%)84.16%

Protein Targets (396)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency13.436019
15-lipoxygenase, partialHomo sapiens (human)Potency15.528816
67.9K proteinVaccinia virusPotency0.449622
acetylcholinesteraseHomo sapiens (human)Potency32.45174133
activating transcription factor 6Homo sapiens (human)Potency17.8433115
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency23.3798124
Alpha-synucleinHomo sapiens (human)Potency10.511212
Amyloid-beta precursor proteinHomo sapiens (human)Potency5.173511
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency14.125411
AR proteinHomo sapiens (human)Potency26.069611154
aryl hydrocarbon receptorHomo sapiens (human)Potency28.7632360
arylsulfatase AHomo sapiens (human)Potency37.933011
ATAD5 protein, partialHomo sapiens (human)Potency12.958434
Ataxin-2Homo sapiens (human)Potency29.8203210
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency20.847223
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency35.1003214
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency13.163812
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency5.211911
beta-2 adrenergic receptorHomo sapiens (human)Potency0.651311
Bloom syndrome protein isoform 1Homo sapiens (human)Potency6.438325
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency44.964712
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency11.287414
caspase-3Cricetulus griseus (Chinese hamster)Potency29.949013
caspase-3Homo sapiens (human)Potency11.287414
Caspase-7Cricetulus griseus (Chinese hamster)Potency29.949013
Cellular tumor antigen p53Homo sapiens (human)Potency39.0168327
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency20.363625
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency35.140615
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency23.735822
Chain A, Beta-lactamaseEscherichia coli K-12Potency62.619023
Chain A, CruzipainTrypanosoma cruziPotency11.669827
Chain A, Ferritin light chainEquus caballus (horse)Potency29.296527
Chain A, HADH2 proteinHomo sapiens (human)Potency22.7088214
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency61.098816
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency5.695416
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.477018
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency38.138726
Chain B, HADH2 proteinHomo sapiens (human)Potency22.7088214
chaperonin-containing TCP-1 beta subunit homologHomo sapiens (human)Potency22.387211
chromobox protein homolog 1Homo sapiens (human)Potency56.326725
core-binding factor subunit beta isoform 2Homo sapiens (human)Potency0.538022
cytochrome P450 2C19 precursorHomo sapiens (human)Potency15.205613
cytochrome P450 2C9 precursorHomo sapiens (human)Potency1.455012
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.393316
cytochrome P450 2D6Homo sapiens (human)Potency8.957017
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency14.274613
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency9.5340234
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency12.2177213
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency35.4298118
D(1A) dopamine receptorHomo sapiens (human)Potency3.264111
D(3) dopamine receptor isoform eHomo sapiens (human)Potency28.183811
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency2.818411
DNA polymerase betaHomo sapiens (human)Potency25.118911
DNA polymerase eta isoform 1Homo sapiens (human)Potency56.234111
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency67.750213
DNA polymerase kappa isoform 1Homo sapiens (human)Potency23.778112
dopamine D1 receptorHomo sapiens (human)Potency5.255212
estrogen nuclear receptor alphaHomo sapiens (human)Potency31.595612147
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency27.5177223
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency29.348710116
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.1469111
EWS/FLI fusion proteinHomo sapiens (human)Potency4.198148
farnesoid X nuclear receptorHomo sapiens (human)Potency25.9624532
flap endonuclease 1Homo sapiens (human)Potency65.344313
Fumarate hydrataseHomo sapiens (human)Potency21.484216
GVesicular stomatitis virusPotency4.393316
GABA theta subunitRattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency9.5340117
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency9.5340117
gemininHomo sapiens (human)Potency11.7930418
GLI family zinc finger 3Homo sapiens (human)Potency16.6354344
glp-1 receptor, partialHomo sapiens (human)Potency14.348412
GLS proteinHomo sapiens (human)Potency16.097529
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency30.7392423
glucokinase regulatory proteinHomo sapiens (human)Potency10.000011
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency36.8378115
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Potency31.622811
Glycoprotein hormones alpha chainHomo sapiens (human)Potency16.062012
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency1.360912
Guanine nucleotide-binding protein GHomo sapiens (human)Potency27.502023
heat shock protein beta-1Homo sapiens (human)Potency27.2955222
hexokinase-4 isoform 1Homo sapiens (human)Potency10.000011
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency7.4828216
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency25.723219
histone deacetylase 9 isoform 3Homo sapiens (human)Potency12.298527
Histone H2A.xCricetulus griseus (Chinese hamster)Potency55.0151226
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency29.881612
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.393316
huntingtin isoform 2Homo sapiens (human)Potency6.691812
hypothetical protein, conservedTrypanosoma bruceiPotency16.826248
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency27.1838217
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency18.380833
IDH1Homo sapiens (human)Potency6.772013
importin subunit beta-1 isoform 1Homo sapiens (human)Potency30.615623
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.3933112
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency14.147628
Integrin alpha-IIbHomo sapiens (human)Potency18.915613
Integrin beta-3Homo sapiens (human)Potency18.915613
Interferon betaHomo sapiens (human)Potency13.1850317
interleukin 8Homo sapiens (human)Potency43.978012
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency51.119012
lamin isoform A-delta10Homo sapiens (human)Potency11.6431213
lethal factor (plasmid)Bacillus anthracis str. A2012Potency12.533113
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency22.106012
LuciferasePhotinus pyralis (common eastern firefly)Potency36.1392326
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency10.000011
luteinizing hormone receptorHomo sapiens (human)Potency84.921411
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency35.481311
M-phase phosphoprotein 8Homo sapiens (human)Potency20.811412
Microtubule-associated protein tauHomo sapiens (human)Potency13.4363217
mitogen-activated protein kinase 1Homo sapiens (human)Potency16.904027
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency14.651524
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency14.315113
neuropeptide S receptor isoform AHomo sapiens (human)Potency9.822635
NFKB1 protein, partialHomo sapiens (human)Potency7.079522
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency10.580813
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency29.8887474
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency13.318114
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency7.765013
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency25.7252115
Nuclear receptor ROR-gammaHomo sapiens (human)Potency42.551514
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency5.6962214
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency24.9430398
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency25.118911
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency19.952611
ParkinHomo sapiens (human)Potency39.810711
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency56.234111
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency11.8879212
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency11.995511
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.6914536
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency20.6273515
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency17.782811
phosphopantetheinyl transferaseBacillus subtilisPotency37.0593313
PINK1Homo sapiens (human)Potency39.810711
plasminogen precursorMus musculus (house mouse)Potency7.414012
polyproteinZika virusPotency21.484216
polypyrimidine tract-binding protein 1 isoform aHomo sapiens (human)Potency14.550022
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency12.129114
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency11.099415
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency29.175016
PPM1D proteinHomo sapiens (human)Potency14.577516
pregnane X nuclear receptorHomo sapiens (human)Potency39.5066351
pregnane X receptorRattus norvegicus (Norway rat)Potency36.881016
progesterone receptorHomo sapiens (human)Potency19.6696230
pyruvate kinaseLeishmania mexicana mexicanaPotency15.848922
pyruvate kinase PKM isoform aHomo sapiens (human)Potency39.810722
pyruvate kinase PKM isoform bHomo sapiens (human)Potency25.118922
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency16.803712
RAR-related orphan receptor gammaMus musculus (house mouse)Potency29.2006234
regulator of G-protein signaling 4Homo sapiens (human)Potency12.863514
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency31.8600359
retinoid X nuclear receptor alphaHomo sapiens (human)Potency27.1336447
runt-related transcription factor 1 isoform AML1bHomo sapiens (human)Potency0.538022
serine-protein kinase ATM isoform aHomo sapiens (human)Potency18.382845
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency0.736033
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency17.287614
SMAD family member 2Homo sapiens (human)Potency18.455929
SMAD family member 3Homo sapiens (human)Potency18.455929
Smad3Homo sapiens (human)Potency3.472113
snurportin-1Homo sapiens (human)Potency30.615623
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency20.991014
survival motor neuron protein isoform dHomo sapiens (human)Potency15.715416
T cell receptor, partialHomo sapiens (human)Potency6.284111
TAR DNA-binding protein 43Homo sapiens (human)Potency18.816014
TDP1 proteinHomo sapiens (human)Potency10.6517233
thioredoxin glutathione reductaseSchistosoma mansoniPotency31.622811
thioredoxin reductaseRattus norvegicus (Norway rat)Potency17.755027
ThrombopoietinHomo sapiens (human)Potency0.398122
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency40.0293336
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency21.0940816
thyroid stimulating hormone receptorHomo sapiens (human)Potency28.6280781
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency23.526723
TSHR proteinHomo sapiens (human)Potency15.503522
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.414012
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.414012
USP1 protein, partialHomo sapiens (human)Potency47.382416
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency25.1243234
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency20.6134523
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency34.4882117
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency36.8378115
VprHuman immunodeficiency virus 1Potency29.293813
WRNHomo sapiens (human)Potency35.481311

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
1-acylglycerol-3-phosphate O-acyltransferase ABHD5 isoform aHomo sapiens (human)IC504.290522
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC507.420011
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC5034.547011
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki21.984011
5-hydroxytryptamine receptor 6Homo sapiens (human)IC5016.001011
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki7.429011
Acetylcholine receptor subunit epsilonHomo sapiens (human)IC500.032411
Acetylcholine receptor subunit epsilonRattus norvegicus (Norway rat)IC509.000011
AcetylcholinesteraseAnopheles gambiae (African malaria mosquito)IC500.192022
AcetylcholinesteraseElectrophorus electricus (electric eel)IC507.8476254314
AcetylcholinesteraseGallus gallus (chicken)IC500.020011
AcetylcholinesteraseHomo sapiens (human)IC508.0551244332
AcetylcholinesteraseMus musculus (house mouse)IC504.19381415
AcetylcholinesteraseRattus norvegicus (Norway rat)IC502.44833850
AcetylcholinesteraseTetronarce californica (Pacific electric ray)IC5012.00731416
AcetylcholinesteraseElectrophorus electricus (electric eel)Ki0.66371010
AcetylcholinesteraseHomo sapiens (human)Ki8.27642227
AcetylcholinesteraseMus musculus (house mouse)Ki1.976723
AcetylcholinesteraseTetronarce californica (Pacific electric ray)Ki16.095012
Acetylcholinesterase Bos taurus (cattle)IC500.90641115
Acetylcholinesterase Drosophila melanogaster (fruit fly)IC501.830011
Acetylcholinesterase Bos taurus (cattle)Ki0.002922
Acyl-CoA desaturase 1Rattus norvegicus (Norway rat)IC501.710011
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC500.013412
Adenosine receptor A3Homo sapiens (human)IC500.356011
Adenosine receptor A3Homo sapiens (human)Ki0.201011
Aldehyde dehydrogenase, mitochondrialHomo sapiens (human)IC503.400011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC5070.370011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki69.812011
Aldo-keto reductase family 1 member C2 Homo sapiens (human)IC506.710011
Aldo-keto reductase family 1 member C3Homo sapiens (human)IC504.990022
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC500.571033
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Ki0.201011
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC500.571033
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Ki0.201011
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC500.678522
Alpha-2A adrenergic receptorHomo sapiens (human)IC504.904011
Alpha-2A adrenergic receptorHomo sapiens (human)Ki1.839011
Alpha-2B adrenergic receptorHomo sapiens (human)IC503.218011
Alpha-2B adrenergic receptorHomo sapiens (human)Ki1.469011
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50465.951044
Amine oxidase [flavin-containing] A Bos taurus (cattle)IC50828.000011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)IC50214.931248
Amine oxidase [flavin-containing] BHomo sapiens (human)IC5017.733333
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)IC50124.607157
Amyloid-beta precursor proteinHomo sapiens (human)IC500.261022
Angiotensin-converting enzyme 2 Homo sapiens (human)IC509.350011
apelin receptorHomo sapiens (human)IC502.630011
Apoptotic peptidase activating factor 1Homo sapiens (human)IC5057.750022
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000014
ATP-dependent translocase ABCB1Homo sapiens (human)IC5034.850011
Beta-secretase 1Homo sapiens (human)IC503.303367
bifunctional UDP-N-acetylglucosamine pyrophosphorylase/glucosamine-1-phosphate N-acetyltransferaseMycobacterium tuberculosis H37RvIC5085.030011
Bile salt export pumpHomo sapiens (human)IC50219.255649
Bile salt export pumpRattus norvegicus (Norway rat)IC50759.650012
C-C chemokine receptor type 2Homo sapiens (human)IC502.468011
C-C chemokine receptor type 2Homo sapiens (human)Ki0.954011
C-C chemokine receptor type 4Homo sapiens (human)IC508.395011
C-C chemokine receptor type 4Homo sapiens (human)Ki4.397011
C-C chemokine receptor type 5Homo sapiens (human)IC5023.661011
C-C chemokine receptor type 5Homo sapiens (human)Ki18.284011
C-X-C chemokine receptor type 2Homo sapiens (human)IC506.013011
C-X-C chemokine receptor type 2Homo sapiens (human)Ki4.209011
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC5036.000011
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000014
Carbamate kinaseGiardia intestinalisIC500.600011
Carbonic anhydrase 1Homo sapiens (human)Ki61.700011
Carbonic anhydrase 12Homo sapiens (human)Ki9.520011
Carbonic anhydrase 13Homo sapiens (human)Ki4.230011
Carbonic anhydrase 14Homo sapiens (human)Ki4.140011
Carbonic anhydrase 2Homo sapiens (human)Ki200.000011
Carbonic anhydrase 3Homo sapiens (human)Ki4.620011
Carbonic anhydrase 4Homo sapiens (human)Ki5.480011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki5.090011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki3.410011
Carbonic anhydrase 6Homo sapiens (human)Ki2.230011
Carbonic anhydrase 7Homo sapiens (human)Ki4.680011
Carbonic anhydrase 9Homo sapiens (human)Ki6.410011
Carboxylic ester hydrolase Equus caballus (horse)IC507.15141417
Carboxylic ester hydrolase Musca domestica (house fly)IC509.510011
Carboxylic ester hydrolase Plutella xylostella (diamondback moth)IC501,355.500022
Carboxylic ester hydrolase Rattus norvegicus (Norway rat)IC5012.99581619
Carboxylic ester hydrolase Equus caballus (horse)Ki3.093333
Caspase-1Homo sapiens (human)IC501.800011
caspase-3 isoform a preproproteinHomo sapiens (human)IC5017.000011
caspase-9 isoform alpha precursorHomo sapiens (human)IC5017.000011
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)IC50100.000011
Chain A, ACETYLCHOLINESTERASETetronarce californica (Pacific electric ray)IC500.506012
Chain E, Fibrin beta chainHomo sapiens (human)IC5046.265522
Choline O-acetyltransferase Rattus norvegicus (Norway rat)IC500.005311
CholinesteraseCanis lupus familiaris (dog)IC506.270011
CholinesteraseEquus caballus (horse)IC507.8788177201
CholinesteraseHomo sapiens (human)IC50216,097,029,848.7245148202
CholinesteraseMus musculus (house mouse)IC500.842055
CholinesteraseEquus caballus (horse)Ki3.293733
CholinesteraseHomo sapiens (human)Ki25.1591810
CruzipainTrypanosoma cruziIC5070.000022
Cytochrome P450 1A2Homo sapiens (human)IC504.000011
Cytochrome P450 1B1Homo sapiens (human)IC504.541044
Cytochrome P450 1B1Homo sapiens (human)Ki0.044011
Cytochrome P450 2D6Homo sapiens (human)IC500.265513
Cytochrome P450 3A4Homo sapiens (human)IC5033.705022
D(1A) dopamine receptorHomo sapiens (human)IC502.158011
D(1A) dopamine receptorHomo sapiens (human)Ki260.359723
D(2) dopamine receptorHomo sapiens (human)IC5023.018011
D(2) dopamine receptorHomo sapiens (human)Ki83.836522
D(3) dopamine receptorHomo sapiens (human)IC501.084011
D(3) dopamine receptorHomo sapiens (human)Ki0.368011
D(4) dopamine receptorHomo sapiens (human)IC503.150011
D(4) dopamine receptorHomo sapiens (human)Ki1.105011
Delta-type opioid receptorMus musculus (house mouse)IC5014.631715
Dihydrolipoyl dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)IC501,000.000011
Dihydrolipoyl dehydrogenase, mitochondrialSus scrofa (pig)IC501,000.000011
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50141.026033
Fructose-1,6-bisphosphatase 1Homo sapiens (human)IC50101.23801010
Gasdermin-DHomo sapiens (human)IC500.400011
Gasdermin-DMus musculus (house mouse)IC500.400011
glucose-6-phosphate 1-dehydrogenase isoform bHomo sapiens (human)IC5080.000011
glucose-6-phosphate dehydrogenase-6-phosphogluconolactonasePlasmodium bergheiIC5056.700033
Glutathione reductasePlasmodium falciparum 3D7IC506.400011
Glutathione reductase, mitochondrialHomo sapiens (human)IC5016.200022
Glycogen synthase kinase-3 betaHomo sapiens (human)IC5037.000033
guanine nucleotide-binding protein subunit alpha-15Homo sapiens (human)IC5029.902011
Histamine H3 receptorHomo sapiens (human)IC500.350011
Histone-lysine N-methyltransferase EHMT1Homo sapiens (human)IC501.600011
Histone-lysine N-methyltransferase EHMT2Homo sapiens (human)IC500.600011
integrase, partialHuman immunodeficiency virus 1IC5019.240522
kallikrein-5 preproproteinHomo sapiens (human)IC5050.000011
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC503.200011
Kappa-type opioid receptorHomo sapiens (human)IC506.103011
Kappa-type opioid receptorHomo sapiens (human)Ki2.441011
large T antigenBetapolyomavirus macacaeIC5010.730011
lens epithelium-derived growth factor p75Homo sapiens (human)IC5019.240522
Liver carboxylesterase 1Homo sapiens (human)IC50100.000011
Lysine-specific demethylase 5AHomo sapiens (human)IC5010.000011
Lysine-specific histone demethylase 1AHomo sapiens (human)IC506.970011
Lysyl oxidase homolog 2Homo sapiens (human)IC500.150011
Lysyl oxidase homolog 3Homo sapiens (human)IC500.093011
Lysyl oxidase homolog 4Homo sapiens (human)IC500.059011
Microtubule-associated protein tauHomo sapiens (human)IC509.425044
Mitogen-activated protein kinase 3 Homo sapiens (human)IC501.510011
Monoglyceride lipaseHomo sapiens (human)IC500.809522
Mu-type opioid receptorHomo sapiens (human)IC503.511011
Mu-type opioid receptorHomo sapiens (human)Ki1.425011
Multidrug resistance-associated protein 4Homo sapiens (human)IC50117.975014
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50160.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC503.000011
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC5035.350022
NeuraminidaseInfluenza A virus (A/Puerto Rico/8/1934(H1N1))Ki14.300011
neutrophil cytosol factor 1Homo sapiens (human)IC500.390011
perilipin-1Homo sapiens (human)IC506.959011
perilipin-5Homo sapiens (human)IC501.622011
Phenylethanolamine N-methyltransferaseBos taurus (cattle)Ki294.000011
polyadenylate-binding protein 1Homo sapiens (human)IC5066.000022
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC5016.066011
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50185.2210815
Procathepsin LHomo sapiens (human)IC509.350011
Prolyl endopeptidaseHomo sapiens (human)IC50162.333323
Protein-lysine 6-oxidaseHomo sapiens (human)IC500.320011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC509.350011
Replicase polyprotein 1abBetacoronavirus England 1IC5018.075022
Replicase polyprotein 1abHuman coronavirus 229EIC509.350011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC506.917199
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC509.350022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki3.710011
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi3.710011
Retinal dehydrogenase 1Homo sapiens (human)IC500.130011
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)Ki0.014622
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.014622
Small conductance calcium-activated potassium channel protein 3Rattus norvegicus (Norway rat)IC5012.700011
Sodium-dependent dopamine transporter Homo sapiens (human)IC504.637011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki3.684011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC5070.370011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki69.812011
Sodium-dependent serotonin transporterHomo sapiens (human)IC50500.500022
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)IC501.000011
Spike glycoproteinBetacoronavirus England 1IC509.350011
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC509.350011
Sterol O-acyltransferase 1Homo sapiens (human)IC500.500011
Sterol O-acyltransferase 1Rattus norvegicus (Norway rat)IC500.500011
Telomerase reverse transcriptaseHomo sapiens (human)IC5037.000011
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)IC5030.000011
trace amine-associated receptor 1Homo sapiens (human)IC500.881811
Transmembrane protease serine 2Homo sapiens (human)IC509.350011
type-1 angiotensin II receptorHomo sapiens (human)IC506.637011
Tyrosine-protein kinase SYKHomo sapiens (human)IC500.160011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC5067.000011
Vascular endothelial growth factor receptor 1 Homo sapiens (human)IC500.590011
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC500.590011
Vascular endothelial growth factor receptor 3Homo sapiens (human)IC500.590011
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC5034.300011
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC5034.300011
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC5034.300011
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC5034.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)Kd8.322023
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 3AHomo sapiens (human)EC5026.000011
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)Kd8.511412
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)Kd8.511412
AcetylcholinesteraseHomo sapiens (human)EC500.571512
AcetylcholinesteraseHomo sapiens (human)Kd0.008011
AcetylcholinesteraseMus musculus (house mouse)Kd50.000022
Beta-secretase 1Homo sapiens (human)Kd2,000.000011
CholinesteraseEquus caballus (horse)Kd1.150011
guanine nucleotide-binding protein subunit alpha-15Homo sapiens (human)EC5029.902011
LacZ protein (plasmid)Escherichia coliEC5040.000011
Microtubule-associated protein tauHomo sapiens (human)EC500.360022
ORF73Human gammaherpesvirus 8EC5075.000011
POsterior SegregationCaenorhabditis elegansEC50186.681011
recombinase AMycobacterium tuberculosis H37RvEC5078.650022
Sodium-dependent noradrenaline transporter Homo sapiens (human)EC50113.886011
Trace amine-associated receptor 1Homo sapiens (human)EC500.493744
Trace amine-associated receptor 1Mus musculus (house mouse)EC500.280011
Trace amine-associated receptor 1Rattus norvegicus (Norway rat)EC500.049522
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)EC503.000011
Zinc finger protein mex-5Caenorhabditis elegansEC50113.886011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcetylcholinesteraseElectrophorus electricus (electric eel)K0.034311
AcetylcholinesteraseHomo sapiens (human)Kc0.250011
AcetylcholinesteraseHomo sapiens (human)MIC0.000011
AlbuminBos taurus (cattle)Kdiss2.900011
Amine oxidase [flavin-containing] AHomo sapiens (human)Km514.000011
Amine oxidase [flavin-containing] BHomo sapiens (human)Km104.700011
Caspase 6, apoptosis-related cysteine peptidaseHomo sapiens (human)AC501.600011
CholinesteraseEquus caballus (horse)K0.120833
D(1A) dopamine receptorHomo sapiens (human)KL390.000011
Dihydrolipoyl dehydrogenase Plasmodium falciparum (malaria parasite P. falciparum)Km49.000011
Dihydrolipoyl dehydrogenase, mitochondrialSus scrofa (pig)Km28.000011
DNA repair protein RAD52 homolog isoform aHomo sapiens (human)AC500.936011
Dopamine beta-hydroxylase Bos taurus (cattle)Km2,000.000011
Glutathione reductase, mitochondrialHomo sapiens (human)Km6.300011
H3 histone acetyltransferaseCandida albicans SC5314AC503.260011
heat shock protein 90, putativePlasmodium falciparum 3D7AC504.554011
heat shock protein HSP 90-alpha isoform 2Homo sapiens (human)AC505.178011
Histamine H3 receptorRattus norvegicus (Norway rat)Km104.700011
hypothetical protein CAALFM_CR05890CACandida albicans SC5314AC503.260011
Polyphenol oxidase 2Agaricus bisporusKm540.000011
POU domain, class 2, transcription factor 1Homo sapiens (human)Km26.400011
prostaglandin E2 receptor EP2 subtypeHomo sapiens (human)Active Concentration20.000011
protein AF-9 isoform aHomo sapiens (human)AC504.080011
replicative DNA helicaseMycobacterium tuberculosis H37RvAC5058.180022
Solute carrier family 22 member 1 Homo sapiens (human)Activity107.000011
Thioredoxin reductase 1, cytoplasmicHomo sapiens (human)Km95.000011